Delayed release compositions of dimethyl fumarate

Abstract

The present invention relates to delayed release pharmaceutical compositions comprising dimethyl fumarate in the treatment of multiple sclerosis. The delayed release composition of dimethyl fumarate is having particle size (D90) of dimethyl fumarate in the composition is less than 50 μm and composition is manufactured by extrusion-spheronization or layering method.

We claim: 
     
         1 . A delayed release pharmaceutical composition of dimethyl fumarate along with one or more pharmaceutically acceptable excipient, which comprises
 a) Core   b) Optionally seal coating and   c) Enteric coating;   Wherein core is manufactured by either extrusion spheronization or layering method.   
     
     
         2 . The delayed release pharmaceutical composition as claimed in  claim 1 , wherein core is manufactured by extrusion-spheronization method which involves
 a) Mixing dimethyl fumarate with one or more pharmaceutically acceptable excipient and granulating same with one or more solvent.   b) Extrude the wet granulated mass in step (a) by extruder and Spheronize the same in spheronizer to form pellet or core.   
     
     
         3 . The delayed release pharmaceutical composition as claimed in  claim 1 , wherein core is manufactured by layering method which involves
 a) Dispersing or dissolving Dimethyl fumarate in one or more pharmaceutically acceptable excipient and solvent.   b) Coating the solution in step (a) on the inert core to form the core.   
     
     
         4 . The delayed release pharmaceutical composition as claimed in  claim 1 , wherein particle size (D90) of dimethyl fumarate is less than 50 μm in the composition. 
     
     
         5 . The delayed release pharmaceutical composition as claimed in  claim 1 , wherein composition is in the form of pellet, granule, bead, spheroid, capsule, tablet or micro granule. 
     
     
         6 . The delayed release pharmaceutical composition of dimethyl fumarate as claimed in  claim 1 , wherein amount of dimethyl fumarate is ranging from 10 mg to 300 mg. 
     
     
         7 . The delayed release pharmaceutical composition of dimethyl fumarate as claimed in  claim 1 , wherein amount of dimethyl fumarate is 120 mg or 240 mg. 
     
     
         8 . The delayed release pharmaceutical composition of dimethyl fumarate as claimed in  claim 1 , wherein one or more pharmaceutically acceptable excipient is selected from the group consisting of Diluent, Adsorbent, Binder, Plasticizer, solvent, Anti-tacking Agent, seal coating polymer, delayed release polymer and solubilizing agent. 
     
     
         9 . The delayed release pharmaceutical composition of dimethyl fumarate as claimed in  claim 8 , wherein diluent is Microcrystalline Cellulose, Mannitol or mixture thereof; adsorbent is Colloidal Anhydrous Silica; binder is povidone; plasticizer is triethyl citrate; solvent are isopropyl alcohol, dichloromethane or water or mixture thereof; anti-tacking agent is talc or silicon dioxide or mixture thereof, seal coating polymer is hydroxyl propyl methyl cellulose and delayed release polymer is Methacrylic Acid-Ethyl Acrylate Copolymer. 
     
     
         10 . The delayed release pharmaceutical composition of dimethyl fumarate as claimed in  claim 1 , for the treatment of multiple sclerosis.